Nitroimidazole compounds are well-known bioactive substances, and the structural activity relationship has been reported whereby the position of the nitro group within the imidazole ring has a large influence on the activity. This study focuses on synthesising new trypanocidal agents from the hybridisation of metronidazole with different natural phenols (eugenol, dihydroeugenol and guaiacol). Two different coupling methodologies have been explored in order to analyse the influence of the connector on bioactivity: i) classic direct esterification (AD compounds) and ii) “click” chemistry using a triazole connector (AC compounds).

中文翻译：

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甲硝唑与丁子香酚类似物杂交合成新型杀锥虫剂

硝基咪唑化合物是众所周知的生物活性物质，并且已经报道了结构活性关系，其中硝基在咪唑环内的位置对其活性有很大影响。本研究的重点是通过甲硝唑与不同天然酚（丁子香酚、二氢丁子香酚和愈创木酚）的杂交来合成新的杀锥虫剂。为了分析连接器对生物活性的影响，我们探索了两种不同的偶联方法：i）经典的直接酯化（AD 化合物）和 ii）使用三唑连接器（AC 化合物）的“点击”化学。